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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
15 Results for "
HLMs
" in MedChemExpress (MCE) Product Catalog:
Products (15)
15 Results for "HLMs" in MCE Product Catalog:
10
10 Publications Verification
Cat. No.: HY-16667
CAS No.: 353519-63-8
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HLM006474 is a pan E2F inhibitor, which inhibits E2F4 DNA-binding with an IC50 of 29.8 μM in A375 cells.
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1 Cited Publications
MMP-7-IN-1 is a highly potent and selective MMP-7 inhibitor with an IC50 of 10 nM. MMP-7-IN-1 can be used in the research of diseases such as cancer and fibrosis .
Cat. No.: HY-17614
CAS No.: 945531-77-1
Synonyms: SMT C1100; BMN 195; VOX-C1100
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Ezutromid (SMT C1100) is a first-in-class, orally active benzoxazole utrophin modulator with an EC50 of 0.91 μM. Ezutromid can be used for the research Duchenne muscular dystrophy (DMD). Ezutromid inhibits CYP1A2 enzymic activity in human liver microsomes (HLM) with an IC50 of 5.4 μM .
KTX-951 is an orally active PROTAC degrader of IRAK4 and IMiD (Ikaros/Aiolos) substrates (Kd = 3.5 nM). KTX-951 induces IRAK4 degradation, and the degradation efficiency is independent of IRAK4 binding affinity. The DC50 values of KTX-951 for IRAK4, Ikaros and Aiolos are 18 nM, 14 nM and 13 nM, respectively. The IC50 of KTX-951 against OCl-Ly10 CTG is 35 nM. KTX-951 exhibits antitumor activity .
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Cardiovascular Disease Alkaloids Other Alkaloids Ranunculaceae Aconitum carmichaeli Debx. Plants Disease Research Fields
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Cat. No.: HY-114663
CAS No.: 1883284-94-3
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FDU-PB-22 is a new synthetic cannabinoid that is rapidly metabolized in HLM, with a half-life of 12.4 minutes .
Cat. No.: HY-118339
CAS No.: 1065110-43-1
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PF-4479745 is a potent and selective 5-HT2C receptor agonist (EC50: 10 nM, ki: 15 nM). PF-4479745 can be used in the research of cardiovascular disease like hypertension .
Cat. No.: HY-176715
CAS No.: 2981435-59-8
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Kv7.2 activator-1 (Compound 8) is a Kv7.2/3 activator with an EC50 of 178 nM. Kv7.2 activator-1 has a long half-life of 120 minutes in HLM .
Cat. No.: HY-146111
CAS No.: 2667681-57-2
IRAK4-IN-13 (compound 21) is a potent and selective IRAK4 inhibitor with an IC50 of 0.6 nM. IRAK4-IN-13 shows high metabolic clearance with human liver microsomes (HLM) intrinsic clearance is 96 µL/min/mg .
Cat. No.: HY-153970
CAS No.: 1632002-28-8
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URAT1 inhibitor 7 (compound 10f) is a potent URAT1 inhibitor, with an IC50 of 12 nM. URAT1 inhibitor 7 exhibits microsomal stability (HLM <13 µL/min/mg). URAT1 inhibitor 7 also inhibits CYP2C9, with an IC50 of 4.2 μM. URAT1 inhibitor 7 can be used for gout research .
Cat. No.: HY-75368
CAS No.: 905580-86-1
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SRI-31255 is an orally active LRRK2 inhibitor with IC50 values of 520 and 427 nM for human wild-type (WT) and mutant G2019S, respectively. SRI-31255 exerts neuroprotective effects by binding to the ATP-binding pocket of LRRK2, inhibiting kinase activity. SRI-31255 can be used as a lead compound for the development of LRRK2-targeted drugs for the treatment of Parkinson's disease .
Cat. No.: HY-17614R
CAS No.: 945531-77-1
Synonyms: SMT C1100 (Standard); BMN 195 (Standard); VOX-C1100 (Standard)
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Ezutromid (Standard) is the analytical standard of Ezutromid. This product is intended for research and analytical applications. Ezutromid (SMT C1100) is a first-in-class, orally active benzoxazole utrophin modulator with an EC50 of 0.91 μM. Ezutromid can be used for the research Duchenne muscular dystrophy (DMD). Ezutromid inhibits CYP1A2 enzymic activity in human liver microsomes (HLM) with an IC50 of 5.4 μM .
Cat. No.: HY-155141
CAS No.: 3003751-14-9
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hCYP3A4-IN-1 (compound C6) is a potent, orally active hCYP3A4 inhibitor. hCYP3A4-IN-1 shows the IC50 values of 43.93 nM and 153.00 nM against hCYP3A4 in human liver microsomes (HLMs) and CHO-3A4 stably transfected cell line, respectively. hCYP3A4-IN-1 potently inhibits CYP3A4-catalyzed N-ethyl-1,8-naphthalimide (NEN) hydroxylation in a competitive manner (Ki = 30.00 nM) .
Cat. No.: HY-135541
CAS No.: 365462-24-4
Synonyms: YM150 maleate
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Darexaban maleate (YM150 maleate) is a direct factor Xa inhibitor with activity in preventing venous thromboembolism. The major metabolite of Darexaban maleate in humans is Darexaban glucitol, which acts pharmacologically. The glucitolation reaction of Darexaban maleate is mainly catalyzed by UGT1A9 and UGT1A10 in the human liver and intestine. The K(m) value of Darexaban maleate glucitolation in the liver is greater than 250 μM, while in the intestine it exhibits substrate inhibition kinetics with a K(m) value of 27.3 μM. The unbound K(m) value of Darexaban maleate is significantly reduced by the influence of fatty acid-free bovine serum albumin in both HLM and UGT1A9 .
Cat. No.: HY-183584
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ARN25699 is a kinase inhibitor with an IC50 of 5.5 nM against GSK-3β, 2.2 nM against FYN-α, and 242.3 nM against DYRK1A, and it exhibits oral bioavailability. ARN25699 reduces hyperphosphorylation of tau protein and promotes microtubule bundle formation. ARN25699 has a broader kinome inhibitory profile and targets kinases associated with the pathogenic mechanisms linked to Alzheimer's disease. ARN25699 can be used in the research of Alzheimer's disease and related tauopathies .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
